Journal article
Cloning and functional expression of the human glucagon-like peptide-1 (GLP-1) receptor
Endocrinology (Philadelphia), Vol.133(4), pp.1907-1910
10/1993
DOI: 10.1210/endo.133.4.8404634
Abstract
Truncated forms of glucagon-like peptide-1 are the most potent endogenous stimuli of insulin secretion and have powerful antidiabetogenic effects. To determine the structure and coupling mechanisms of the human GLP-1 receptor we have isolated two pancreatic islet cDNAs, encoding the 463 amino acid receptor and differing mainly in their 3' untranslated regions. The deduced amino acid sequence is 90% homologous with the rat GLP-1 receptor. Northern blot analysis shows expression of a single 2.7 kb transcript in pancreatic tissue. When expressed in COS-7 cells the recombinant receptor conferred specific, high affinity GLP-1(7-37) binding. GLP-1(7-37) increased intracellular cAMP in a concentration dependent manner and caused an increase in the free cytosolic calcium ([Ca2+]i) from an intracellular pool, characteristic of phospholipase C (PLC) activation. Thus, like the structurally related glucagon and parathyroid hormone receptors, the human GLP-1 receptor can activate multiple intracellular signaling pathways including adenylyl cyclase and PLC. Knowledge of the GLP-1 receptor structure will facilitate the development of receptor agonists and elucidation of the important role of GLP-1 in normal physiology and disease states.
Details
- Title: Subtitle
- Cloning and functional expression of the human glucagon-like peptide-1 (GLP-1) receptor
- Creators
- J S Dillon - Tufts UniversityY Tanizawa - Tufts UniversityM B Wheeler - Tufts UniversityX H Leng - Tufts UniversityB B Ligon - Tufts UniversityD U Rabin - Tufts UniversityH Yoo-Warren - Tufts UniversityM A Permutt - Tufts UniversityA E Boyd - Tufts University
- Resource Type
- Journal article
- Publication Details
- Endocrinology (Philadelphia), Vol.133(4), pp.1907-1910
- DOI
- 10.1210/endo.133.4.8404634
- ISSN
- 0013-7227
- eISSN
- 1945-7170
- Language
- English
- Date published
- 10/1993
- Academic Unit
- Fraternal Order of Eagles Diabetes Research Center; Endocrinology and Metabolism; Internal Medicine
- Record Identifier
- 9984359932402771
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